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Items: 49

1.

Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.

Papeo G, Orsini P, Avanzi NR, Borghi D, Casale E, Ciomei M, Cirla A, Desperati V, Donati D, Felder ER, Galvani A, Guanci M, Isacchi A, Posteri H, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Montagnoli A.

ACS Med Chem Lett. 2019 Mar 13;10(4):534-538. doi: 10.1021/acsmedchemlett.8b00569. eCollection 2019 Apr 11.

PMID:
30996792
2.

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications.

Ardini E, Menichincheri M, Banfi P, Bosotti R, De Ponti C, Pulci R, Ballinari D, Ciomei M, Texido G, Degrassi A, Avanzi N, Amboldi N, Saccardo MB, Casero D, Orsini P, Bandiera T, Mologni L, Anderson D, Wei G, Harris J, Vernier JM, Li G, Felder E, Donati D, Isacchi A, Pesenti E, Magnaghi P, Galvani A.

Mol Cancer Ther. 2016 Apr;15(4):628-39. doi: 10.1158/1535-7163.MCT-15-0758. Epub 2016 Mar 3.

3.

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M, Fasolini M, Forte B, Galvani A, Isacchi A, Khvat A, Krasavin MY, Lupi R, Orsini P, Perego R, Pesenti E, Pezzetta D, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Sola F, Zuccotto F, Felder ER, Donati D, Montagnoli A.

J Med Chem. 2015 Sep 10;58(17):6875-98. doi: 10.1021/acs.jmedchem.5b00680. Epub 2015 Aug 26.

PMID:
26222319
4.

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.

Brasca MG, Gnocchi P, Nesi M, Amboldi N, Avanzi N, Bertrand J, Bindi S, Canevari G, Casero D, Ciomei M, Colombo N, Cribioli S, Fachin G, Felder ER, Galvani A, Isacchi A, Motto I, Panzeri A, Donati D.

Bioorg Med Chem. 2015 May 15;23(10):2387-407. doi: 10.1016/j.bmc.2015.03.059. Epub 2015 Mar 28.

PMID:
25882525
5.

Optimization of diarylthiazole B-raf inhibitors: identification of a compound endowed with high oral antitumor activity, mitigated hERG inhibition, and low paradoxical effect.

Pulici M, Traquandi G, Marchionni C, Modugno M, Lupi R, Amboldi N, Casale E, Colombo N, Corti L, Fasolini M, Gasparri F, Pastori W, Scolaro A, Donati D, Felder E, Galvani A, Isacchi A, Pesenti E, Ciomei M.

ChemMedChem. 2015 Feb;10(2):276-95. doi: 10.1002/cmdc.201402424. Epub 2014 Nov 27.

PMID:
25430902
6.

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.

Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21.

PMID:
25009002
7.

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.

Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A.

Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14.

8.

Anti-tumour efficacy on glioma models of PHA-848125, a multi-kinase inhibitor able to cross the blood-brain barrier.

Albanese C, Alzani R, Amboldi N, Degrassi A, Festuccia C, Fiorentini F, Gravina G, Mercurio C, Pastori W, Brasca M, Pesenti E, Galvani A, Ciomei M.

Br J Pharmacol. 2013 May;169(1):156-66. doi: 10.1111/bph.12112.

9.

Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.

Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S.

Biochem Pharmacol. 2012 Sep 1;84(5):598-611. doi: 10.1016/j.bcp.2012.06.004. Epub 2012 Jun 13.

PMID:
22704958
10.

Phase I study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies.

Weiss GJ, Hidalgo M, Borad MJ, Laheru D, Tibes R, Ramanathan RK, Blaydorn L, Jameson G, Jimeno A, Isaacs JD, Scaburri A, Pacciarini MA, Fiorentini F, Ciomei M, Von Hoff DD.

Invest New Drugs. 2012 Dec;30(6):2334-43. doi: 10.1007/s10637-011-9774-6. Epub 2011 Dec 9.

11.

Miniaturizing bromodeoxyuridine incorporation enables the usage of flow cytometry for cell cycle analysis of adherent tissue culture cells for high throughput screening.

Cappella P, Giorgini ML, Ernestina Re C, Ubezio P, Ciomei M, Moll J.

Cytometry A. 2010 Oct;77(10):953-61. doi: 10.1002/cyto.a.20962. Epub 2010 Sep 8.

12.

Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.

Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M.

Mol Cancer Ther. 2010 Aug;9(8):2243-54. doi: 10.1158/1535-7163.MCT-10-0190. Epub 2010 Aug 3.

13.

Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study.

Locatelli G, Bosotti R, Ciomei M, Brasca MG, Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Galvani A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A.

Mol Cancer Ther. 2010 May;9(5):1265-73. doi: 10.1158/1535-7163.MCT-09-1163. Epub 2010 Apr 27.

14.

Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging.

Degrassi A, Russo M, Nanni C, Patton V, Alzani R, Giusti AM, Fanti S, Ciomei M, Pesenti E, Texido G.

Mol Cancer Ther. 2010 Mar;9(3):673-81. doi: 10.1158/1535-7163.MCT-09-0726. Epub 2010 Mar 2.

15.

Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models.

Alzani R, Pedrini O, Albanese C, Ceruti R, Casolaro A, Patton V, Colotta F, Rambaldi A, Introna M, Pesenti E, Ciomei M, Golay J.

Exp Hematol. 2010 Apr;38(4):259-269.e2. doi: 10.1016/j.exphem.2010.02.004. Epub 2010 Feb 16.

PMID:
20167248
16.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.

Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25.

PMID:
20153204
17.

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG.

J Med Chem. 2010 Mar 11;53(5):2171-87. doi: 10.1021/jm901710h.

PMID:
20141146
18.

The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound.

Caporali S, Alvino E, Starace G, Ciomei M, Brasca MG, Levati L, Garbin A, Castiglia D, Covaciu C, Bonmassar E, D'Atri S.

Pharmacol Res. 2010 May;61(5):437-48. doi: 10.1016/j.phrs.2009.12.009. Epub 2009 Dec 21.

PMID:
20026273
19.

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M.

J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559.

PMID:
19603809
20.

Antitumor activity of edotecarin in breast carcinoma models.

Ciomei M, Croci V, Stellari F, Amboldi N, Giavarini R, Pesenti E.

Cancer Chemother Pharmacol. 2007 Jul;60(2):229-35. Epub 2006 Nov 7.

PMID:
17089166
21.

Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model.

Ciomei M, Croci V, Ciavolella A, Ballinari D, Pesenti E.

Clin Cancer Res. 2006 May 1;12(9):2856-61.

22.

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14.

PMID:
16290148
23.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C.

J Med Chem. 2005 Apr 21;48(8):2944-56. Erratum in: J Med Chem. 2005 Jul 28;48(15):5058.

PMID:
15828833
24.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.

J Med Chem. 2004 Jun 17;47(13):3367-80.

PMID:
15189033
25.

Multiple effects of paclitaxel are modulated by a high c-myc amplification level.

Bottone MG, Soldani C, Tognon G, Gorrini C, Lazzè MC, Brison O, Ciomei M, Pellicciari C, Scovassi AI.

Exp Cell Res. 2003 Oct 15;290(1):49-59.

PMID:
14516787
26.

Effects of topoisomerase II inhibitors on gastric cancer cells characterized by different genetic lesions.

Scovassi AL, Pellegata NS, Di Stefano L, Padovan L, Negri C, Prosperi E, Riva F, Ciomei M, Ranzani GN.

Anticancer Res. 2001 Jul-Aug;21(4A):2803-8.

PMID:
11724358
27.

Pharmacological and toxicological aspects of 4-demethoxy-3'-deamino-3'-aziridinyl-4'-methylsulphonyl-daunorubicin (PNU-159548): a novel antineoplastic agent.

Geroni C, Ripamonti M, Arrigoni C, Fiorentini F, Capolongo L, Moneta D, Marchini S, Della Torre P, Albanese C, Lamparelli MG, Ciomei M, Rossi R, Caruso M.

Cancer Res. 2001 Mar 1;61(5):1983-90.

28.

Antiangiogenic, antitumoural and antimetastatic effects of two distamycin A derivatives with anti-HIV-1 Tat activity in a Kaposi's sarcoma-like murine model.

Possati L, Campioni D, Sola F, Leone L, Ferrante L, Trabanelli C, Ciomei M, Montesi M, Rocchetti R, Talevi S, Bompadre S, Caputo A, Barbanti-Brodano G, Corallini A.

Clin Exp Metastasis. 1999;17(7):575-82.

PMID:
10845556
29.

Characterization of the effects of two polysulfonated distamycin A derivatives, PNU145156E and PNU153429, on HIV type 1 Tat protein.

Corallini A, Betti M, Rusnati M, Campioni D, Ciomei M, Sola F, Calza N, Zauli G, Presta M, Barbanti-Brodano G, Caputo A.

AIDS Res Hum Retroviruses. 1998 Nov 20;14(17):1561-71.

PMID:
9840289
30.

Synthesis and binding mode of heterocyclic analogues of suramin inhibiting the human basic fibroblast growth factor.

Manetti F, Cappello V, Botta M, Corelli F, Mongelli N, Biasoli G, Borgia AL, Ciomei M.

Bioorg Med Chem. 1998 Jul;6(7):947-58.

PMID:
9730230
31.

The basic domain in HIV-1 Tat protein as a target for polysulfonated heparin-mimicking extracellular Tat antagonists.

Rusnati M, Tulipano G, Urbinati C, Tanghetti E, Giuliani R, Giacca M, Ciomei M, Corallini A, Presta M.

J Biol Chem. 1998 Jun 26;273(26):16027-37.

32.

Anti-insulin-like growth factor-I activity of a novel polysulphonated distamycin A derivative in human lung cancer cell lines.

de Cupis A, Ciomei M, Pirani P, Ferrera A, Ardizzoni A, Favoni RE.

Br J Pharmacol. 1997 Feb;120(3):537-43.

33.

Endothelial cells overexpressing basic fibroblast growth factor (FGF-2) induce vascular tumors in immunodeficient mice.

Sola F, Gualandris A, Belleri M, Giuliani R, Coltrini D, Bastaki M, Tosatti MP, Bonardi F, Vecchi A, Fioretti F, Ciomei M, Grandi M, Mantovani A, Presta M.

Angiogenesis. 1997;1(1):102-116.

PMID:
14517397
34.

Decreased tyrosine phosphorylation in tumour cells resistant to FCE 24517 (tallimustine).

Ciomei M, Pastori W, Capolongo L, Geroni C, Melegaro G, Pennella G, Grandi M.

Br J Cancer. 1995 Dec;72(6):1504-8.

35.

FCE 27266, a sulfonic distamycin derivative, inhibits experimental and spontaneous lung and liver metastasis.

Sola F, Farao M, Ciomei M, Pastori A, Mongelli N, Grandi M.

Invasion Metastasis. 1995;15(5-6):222-31.

PMID:
8765197
36.

New sulfonated distamycin A derivatives with bFGF complexing activity.

Ciomei M, Pastori W, Mariani M, Sola F, Grandi M, Mongelli N.

Biochem Pharmacol. 1994 Jan 20;47(2):295-302.

PMID:
7508230
37.

In vitro and in vivo activity of alkylating bombesin receptor antagonists on small cell lung carcinoma.

Ciomei M, Pastori W, Pastori A, de Castiglione R, Gozzini L, Corradi F.

Anticancer Res. 1993 Jan-Feb;13(1):75-9.

PMID:
8386497
38.

Bombesin receptor antagonists. 5 new irreversible alkylating analogues.

de Castiglione R, Gozzini L, Galantino M, Corradi F, Ciomei M, Roletto F, Bertolero F.

Farmaco. 1992 Jun;47(6):855-67.

PMID:
1326977
39.

Inhibitory effect of suramin on receptor binding and cytotoxic activity of tumor necrosis factor alpha.

Grazioli L, Alzani R, Ciomei M, Mariani M, Restivo A, Cozzi E, Marcucci F.

Int J Immunopharmacol. 1992 May;14(4):637-42.

PMID:
1325955
40.

In vitro activity of novel sulphonic derivatives of distamycin A.

Mariani M, Paio A, Ciomei M, Pastori W, Franzetti C, Melegaro G, Grandi M, Mongelli N.

EXS. 1992;61:455-8.

PMID:
1377571
41.

Bombesin receptor antagonists. 2. Analogues based on substance P antagonists.

Rusconi L, de Castiglione R, Gozzini L, Ciomei M, Molinari I, Basilico L, Rubino T, Vinayek R, Gardner JD.

Farmaco. 1991 Jun;46(6):725-42.

PMID:
1722978
42.

Bombesin receptor antagonists. 3. Irreversible alkylating analogues: melphalan derivatives.

de Castiglione R, Gozzini L, Galantino M, Corradi F, Arlandini E, Molinari I, Ciomei M.

Farmaco. 1991 Jun;46(6):743-57.

PMID:
1663360
43.

Bombesin receptor antagonists [corrected]. 1. Analogues with deleted, inverted or substituted amino acid residues.

De Castiglione R, Gozzini L, Mena R, Brugnolotti M, Ciomei M, Molinari I, Comoglio PM, Gaudino G.

Farmaco. 1990 Dec;45(12):1251-63. Erratum in: Farmaco 1991 Feb;46(2):following 414.

PMID:
1965286
44.

Bombesin stimulates growth of human prostatic cancer cells in vitro.

Bologna M, Festuccia C, Muzi P, Biordi L, Ciomei M.

Cancer. 1989 May 1;63(9):1714-20.

PMID:
2539244
45.
46.

Quantitation of DNA damage in non-radioactive DNA.

Sutherland BM, Ciarrocchi G, Ciomei M, Sutherland JC.

Photochem Photobiol. 1986 Sep;44(3):391-6. No abstract available.

PMID:
3538069
47.

Quantification of pyrimidine dimers and apurinic sites in DNAs of uniform length.

Ciomei M, Sutherland BM, Ciarrocchi G.

Photochem Photobiol. 1984 May;39(5):593-6. No abstract available.

PMID:
6377338
48.

Structural alterations of pathologically or physiologically modified DNA.

Ciomei M, Spadari S, Pedrali-Noy G, Ciarrocchi G.

Nucleic Acids Res. 1984 Feb 24;12(4):1977-89.

49.

DNA methylation and DNA structure.

Spadari S, Pedrali-Noy G, Ciomei M, Rebuzzini A, Hübscher U, Ciarrocchi G.

Adv Exp Med Biol. 1984;179:551-6. No abstract available.

PMID:
6524502

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